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. Author manuscript; available in PMC: 2022 Oct 10.
Published in final edited form as: J Invest Dermatol. 2021 Sep 1;142(3 Pt A):594–602. doi: 10.1016/j.jid.2021.07.178

Figure 4. Characterization of Mrgprs activated by β-defensins.

Figure 4.

(a) FLIPR screening of HEK-293 cells heterologously expressing human MRG receptors revealed that DEFB103 potently activated human MRGPRX1 and MRGPRX2, (b) DEFB4 weakly activated MRGPRX2, and (c) Defb14 potently stimulated mouse Mrgpra1, Mrgpra3 and Mrgprb2. (d-f) The potency for activation of Mrgprs by defensins is related to the net charge values of peptides. (d) Human MRGPRX1 displayed higher affinity for DEFB103 (+10.6) and Defb14 (+11.6) than DEFB4 (+5.7). (e) Mouse Mrgpra1 exhibited higher affinity for Defb14, Defb3 (+10.6), than Defb4 (+6.6) and Defb1 (+5.7). All results are averages from 3–4 replicates ±SEM. (f) DEFB103 and Defb14 exhibited higher potency (≤ 1μM) in activating MGPRX1, MRGPRX2, Mrgpra1, Mrgpra3 and Mrgprb2. By contrast, DEFB4 and Defb4 exhibited low potency (≥ 10μM).